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S82808

ARQ-092

MedMol 98%
  • 英文名:
  • ARQ-092
  • 别名:
  • CAS号:
  • 1313881-70-7
  • 分子式:
  • C27H24N6
  • 分子量:
  • 432.5197
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
MedMol S82808-1mg 98% ¥442.00元 10 - - - EA 加入购物车
MedMol S82808-5mg 98% ¥625.60元 8 - - - EA 加入购物车
MedMol S82808-10mg 98% ¥1190.00元 4 - - - EA 加入购物车
MedMol S82808-50mg 98% ¥4600.00元 2 - - - EA 加入购物车
源叶(MedMol) S82808-100mg 98% ¥7300.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib is effective against Leishmania
  • 靶点: Akt1:2.7 nM (IC50);Leishmania;Akt3:8.1 nM (IC50);Akt2:14 nM (IC50);Akt1 E17K mutant;Akt; Parasite
  • 体外研究:
    In a large panel of cell lines derived from various tumor types, Miransertib (ARQ-092; Compound 21a) shows potent anti-proliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss. Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells. The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31 μM). Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages
  • 体内研究:
    Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t1/2 values of 17 h in rats versus 7 h in monkeys. The Cmax is 198 ng/mL and 258 ng/mL and the AUCinf was 5496 h•ng/mL and 2960 h•ng/mL in rats and monkeys, respectively. Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma
  • 参考文献:
    1. Lapierre JM, et al. Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. J Med Chem. 2016 Jul 14;59(13):6455-69. 2. Devki Nandan, et al. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. PLoS One. 2018 Nov 6;13(11):e0206920.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.312 ml 11.56 ml 23.12 ml
    5 mM 0.462 ml 2.312 ml 4.624 ml
    10 mM 0.231 ml 1.156 ml 2.312 ml
    50 mM 0.046 ml 0.231 ml 0.462 ml
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